| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Anti-inflammatory agent 36 (Compound 5a28) has an IC50 of 3.69 μM for TNF-α and 3.68 μM for IL-6, which inhibits the release of both cytokines from activated RAW 264.7 murine macrophages when exposed to LPS[1]. In RAW 264.7 murine macrophages, LPS-induced P-P38 and P-ERK is inhibited by anti-inflammatory drug 36 (10 μM, 0.5 hours)[1]. Anti-inflammatory drug 36 (10 μM, 0.5 h) suppresses TNF-α, IL-6, IL-1β, ICAM-1, and VCAM-1 transcription that is triggered by LPS [1].
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|---|---|
| ln Vivo |
In a mouse model of acute lung injury, anti-inflammatory drug 36 (compound 5a28) (10 mg/kg, intraperitoneal injection) reduces inflammation[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW 264.7 mouse macrophages Tested Concentrations: 10 μM Incubation Duration: 0.5 h Experimental Results: Markedly inhibited P-P38 and P-ERK, indicating the suppression of MAPK signaling. |
| Animal Protocol |
Animal/Disease Models: Acute lung injury mouse model[1]
Doses: 10 mg/kg Route of Administration: ip Experimental Results: decreased wet/dry weight ratio of the mice lungs. decreased biomarkers of lymphocytes and macrophages. Suppresses TNF-α, IL-6, IL -1β, 7 VACM-1 and ICAM-1 levels. |
| References |
[1]. Qian J, et al. Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). Eur J Med Chem. 2019 Apr 1;167:414-425.
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| Molecular Formula |
C25H27NO7
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|---|---|
| Molecular Weight |
453.48
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| Exact Mass |
453.178
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| CAS # |
2293951-01-4
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| PubChem CID |
155521683
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
722
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=CC(=C1OC)OC)/C=C/2\CCCN(C2=O)C(=O)/C=C/C3=CC(=C(C=C3)O)OC
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| InChi Key |
XQUXWWVMQPNGGF-KWKAUDIHSA-N
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| InChi Code |
InChI=1S/C25H27NO7/c1-30-20-13-16(7-9-19(20)27)8-10-23(28)26-11-5-6-18(25(26)29)12-17-14-21(31-2)24(33-4)22(15-17)32-3/h7-10,12-15,27H,5-6,11H2,1-4H3/b10-8+,18-12+
|
| Chemical Name |
(3E)-1-[(E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enoyl]-3-[(3,4,5-trimethoxyphenyl)methylidene]piperidin-2-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (55.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2052 mL | 11.0258 mL | 22.0517 mL | |
| 5 mM | 0.4410 mL | 2.2052 mL | 4.4103 mL | |
| 10 mM | 0.2205 mL | 1.1026 mL | 2.2052 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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